01358nas a2200229   4500000000100000008004100001260001700042653001600059653001100075653001100086653001200097653000900109653002300118100001300141700001700154700001700171245005100188300001000239490000600249520085900255022001401114       1981                            d  c1981 Nov-Dec10aClofazimine10aFemale10aHumans10aleprosy10aMale10aModels, Biological1 aFeng P C1 aFenselau C C1 aJacobson R R00aMetabolism of clofazimine in leprosy patients.  a521-40 v93 a<p>We have identified two metabolites of clofazimine (B663; Lamprene; 3-(p-chloroanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine)  in our initial investigation of its metabolism in leprosy patients. Based on mass, ultraviolet, and visible spectrometry, we characterized an unconjugated (metabolite I, 3-(p-hydroxyanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine ) and a conjugated (metabolite II, 3-(beta-D-glucopyranosiduronic acid)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine) metabolite from the urine of patients. Both metabolites were red in color, similar to clofazimine; however, both were considerably more polar than the parent drug. We suggest that metabolite I was formed by a hydrolytic dehalogenation reaction, and metabolite II by hydrolytic deamination followed by glucuronidation.</p>  a0090-9556